論文

査読有り 最終著者 責任著者 国際誌
2021年7月

Development of ciclesonide analogues that block SARS-CoV-2 RNA replication

Bioorganic & Medicinal Chemistry Letters
  • Genichiro Tsuji
  • ,
  • Kenzo Yonemitsu
  • ,
  • Takahito Ito
  • ,
  • Yuta Yanase
  • ,
  • Masashi Uema
  • ,
  • Nobumichi Ohoka
  • ,
  • Takao Inoue
  • ,
  • Hiroshi Asakura
  • ,
  • Yosuke Demizu

43
開始ページ
128052
終了ページ
128052
記述言語
英語
掲載種別
研究論文(学術雑誌)
DOI
10.1016/j.bmcl.2021.128052
出版者・発行元
Elsevier {BV}

Ciclesonide is an inhaled corticosteroid used to treat asthma and is currently undergoing clinical trials for treatment of coronavirus disease 2019 (COVID-19). An active metabolite of ciclesonide, Cic2, was recently reported to repress severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) genomic RNA replication. Herein, we designed and synthesized a few types of ciclesonide analogues. Cic4 (bearing an azide group) and Cic6 (bearing a chloro group) potently decreased SARS-CoV-2 viral replication and had low cytotoxicity compared with Cic2 (bearing a hydroxy group). These compounds are promising as novel therapeutic agents for COVID-19 that show significant antiviral activity.

リンク情報
DOI
https://doi.org/10.1016/j.bmcl.2021.128052
PubMed
https://www.ncbi.nlm.nih.gov/pubmed/33887440
PubMed Central
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8055493
Web of Science
https://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=JSTA_CEL&SrcApp=J_Gate_JST&DestLinkType=FullRecord&KeyUT=WOS:000663580200005&DestApp=WOS_CPL
ID情報
  • DOI : 10.1016/j.bmcl.2021.128052
  • ISSN : 0960-894X
  • eISSN : 1464-3405
  • ORCIDのPut Code : 92509672
  • PubMed ID : 33887440
  • PubMed Central 記事ID : PMC8055493
  • Web of Science ID : WOS:000663580200005

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